2-Hydroxy-4-isopropylbenzaldehyde, a potent partial tyrosinase inhibitor

被引：43
作者：
Nihei, K
Yamagiwa, Y
Kamikawa, T
Kubo, I [1 ]
机构：
[1] Univ Calif Berkeley, Dept Environm Sci Policy & Management, Berkeley, CA 94720 USA
[2] Kinki Univ, Fac Sci & Technol, Dept Chem, Higashiosaka, Osaka 5778502, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 03期
关键词：
mushroom tyrosinase; benzaldehydes; chamaecin; Vilsmeier reaction; partial mixed type inhibitor;
D O I：
10.1016/j.bmcl.2003.11.033
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Chamaecin (2-hydroxy-4-isopropylbenzaldehyde) was synthesized and tested for its tyrosinase inhibitory activity. It partially inhibits the oxidation Of L-3,4-dihydroxyphenylalanine (L-DOPA) catalyzed by mushroom tyrosinase with an IC50 of 2.3 muM. The inhibition kinetics analyzed by Dixon plots found that chamaecin is a mixed type inhibitor. This inhibition may come in part from its ability to form a Schiff base with a primary amino group in the enzyme. (C) 2003 Elsevier Ltd. All rights reserved.
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页码：681 / 683
页数：3
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